Visible-light mediated oxidative ring expansion of anellated cyclopropanes to fused endoperoxides with antimalarial activity

Visible-light mediated oxidative ring expansion of anellated cyclopropanes to fused endoperoxides with antimalarial activity
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DOI:
10.1039/d0qo00168f
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发表时间:
2020-07-21
影响因子:
5.4
通讯作者:
Reiser, Oliver
Reiser, Oliver
中科院分区:
化学1区
文献类型:
--
作者:
Budde, Simon;Goerdeler, Felix;Reiser, Oliver

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在可见光的作用下,分子氧在常压下对碳链和杂环的环丙烷进行扩环反应。由于耐受各种官能团,反应产物融合了1,2-二氧杂环戊烷,由于它们与青蒿素等批准药物的活性成分非常相似,因此对它们进行了抗疟疾活性测试。
A visible light mediated ring expansion of readily available carbo- and heterocyclic anellated cyclopropanes by molecular oxygen at ambient pressure has been developed. Tolerating a variety of functional groups, the reaction yields fused 1,2-dioxolanes, which were tested for antimalarial activity given their close analogy to the active principle of approved drugs such as artemisinin.